title: Synthesis and in vitro cytostatic activity of 1,2- and 1,3-diacylglycerophosphates of clofarabine.
abstract: The conjugates of anticancer nucleoside clofarabine [2-chloro-9-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)adenine] with 1,2- and 1,3-diacylglycerophosphates have been prepared by the phosphoramidite method using a combination of 1,1,3,3-tetraisopropyldisiloxane-1,3-diyl protecting group for the sugar moiety of the nucleoside and 2-cyanoethyl protection for the phosphate fragment. Some of the synthesized conjugates exhibited cytostatic activity against HL-60, A-549, MCF-7, and HeLa tumor cell lines.
authors.affiliation: Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, BY-220141 Minsk, Belarus. ilonaolenikova@tut.by
authors.forename: Ilona
authors.initials: I
authors.lastname: Tsybulskaya
authors.forename: Tamara
authors.initials: T
authors.lastname: Kulak
authors.forename: Alexander
authors.initials: A
authors.lastname: Baranovsky
authors.forename: Marina
authors.initials: M
authors.lastname: Golubeva
authors.forename: Boleslav
authors.initials: B
authors.lastname: Kuzmitsky
authors.forename: Elena
authors.initials: E
authors.lastname: Kalinichenko
mesh_terms: D000227:Adenine Nucleotides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001087:Arabinonucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D000077866:Clofarabine; D054697:Cytostatic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005994:Glycerophosphates / Q000737:chemistry*; D018922:HL-60 Cells; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells
chemical_list: D000227:Adenine Nucleotides; D001087:Arabinonucleosides; D054697:Cytostatic Agents; D005994:Glycerophosphates; D000077866:Clofarabine
keywords: 1,2-, 1,3-Diacylglycerophospholipids; Antitumor activity; Clofarabine; Phosphoramidite approach; Prodrugs